Aqueous formulation containing a piperidinylcyclopentylheptenoic acid derivative and beta-cyclodextrin

Abstract

Aqueous formulations comprising [1R-[1α(Z),2β,3β,5α]]-(+)-7-[5-[[(1,1'-biphenyl)-4-yl]methoxy]-3-hydroxy-2-(1-piperidinyl) cyclopentyl]-4-heptenoic acid or its hydrochloride salt and an unsubstituted or substituted α-, β- or γ-cyclodextrin have been found which are particularly useful in the treatment or prophylaxis of conditions mediated by thromboxane A 2 . Suitable aqueous formulations include injections, oral preparations such as syrups and capsules and inhalation preparations.

We claim: 
     
       1. A clear aqueous formulation comprising the hydrochloride salt of [1R-[1α(Z),2β,3β,5α]]-(+)-7-[5-[[1,1'-biphenyl)-4-yl]methoxy]-3-hydroxy-2-(1-piperidinyl)cyclopentyl]-4-heptenoic acid (Compound A) and β-cyclodextrin or a hydrate thereof, at a pH of about 6.0, wherein the formulation comprises about 1.4 moles of β-cyclodextrin for every 1 mole of the hydrochloride salt of Compound A and wherein the formulation comprises at least 1 mg./ml. of the salt of Compound A expressed as the free base. 
     
     
       2. A formulation as claimed in claim 1 which also comprises sodium hydroxide. 
     
     
       3. A method of treating occlusive vascular diseases and peri- and post-operative complications following organ transplantation, coronary artery bypass, peripheral artery bypass and thrombosis in a human or non-human animal body, which method comprises administering to said body a pharmaceutically effective amount of the formulation as claimed in claim 1.